公开(公告)号：US4880801A

公开(公告)日：1989-11-14

申请号：US198971

申请日：1988-05-26

申请人： John Kitchin ,  Peter C. Cherry ,  Adrian J. Pipe ,  Andrew J. Crame ,  Alan D. Borthwick

发明人： John Kitchin ,  Peter C. Cherry ,  Adrian J. Pipe ,  Andrew J. Crame ,  Alan D. Borthwick

IPC分类号： A61K31/40 ,  A61P1/12 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  A61P7/02 ,  A61P9/12 ,  A61P25/04 ,  A61P25/06 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D319/20 ,  C07D491/04 ,  C07D491/056

CPC分类号： C07D491/04 ,  C07D319/20

摘要： Compounds of the general formula (I) ##STR1## (R is H, alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or CHO, R.sup.1 and R.sup.2 are independently halogen, alkyl, alkoxy, hydroxyl, cyano, nitro or --NR.sup.3 R.sup.4 where R.sup.3 and R.sup.4 are independently H or alkyl and R.sup.2 may be H) and their salts have selective .alpha..sub.2 -adrenoreceptor antagonist action.The compounds may be prepared by amination of compounds of the general formula (II) ##STR2## (where R.sup.1 and R.sup.2 are as defined above and X is a leaving group.

公开(公告)号：US4769367A

公开(公告)日：1988-09-06

申请号：US878263

申请日：1986-06-25

申请人： Peter C. Cherry ,  Adrian J. Pipe ,  John Kitchin ,  Alan D. Borthwick ,  Richard J. Coles ,  Derek Burn

发明人： Peter C. Cherry ,  Adrian J. Pipe ,  John Kitchin ,  Alan D. Borthwick ,  Richard J. Coles ,  Derek Burn

IPC分类号： C07D311/58 ,  C07D311/66 ,  C07D491/04 ,  C07D491/052 ,  A61K31/55 ,  A61K31/40 ,  C07D209/56

CPC分类号： C07D491/04 ,  C07D311/58 ,  C07D311/66

摘要： Compounds of the general formula (I) ##STR1## (wherein R is H, alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or CHO; and R.sup.1 and R.sup.2 each represents H, fluorine or chlorine);and their salts have selective .alpha..sub.2 -adrenoreceptor antagonist action.The compounds may be prepared by amination of compounds of the general formula (II): ##STR2## (wherein X is a leaving group).

摘要翻译： 通式（I）的化合物（I）（其中R是H，烷基，烯基，炔基，环烷基，芳烷基或CHO; R 1和R 2各自表示H，氟或氯）。 并且它们的盐具有选择性的α2-肾上腺素受体拮抗作用。 化合物可以通过通式（II）的化合物的胺化来制备：其中X是离去基团。

公开(公告)号：US4228074A

公开(公告)日：1980-10-14

申请号：US831549

申请日：1977-09-08

申请人： Peter C. Cherry ,  Christopher E. Newall ,  Nigel S. Watson

发明人： Peter C. Cherry ,  Christopher E. Newall ,  Nigel S. Watson

IPC分类号： C07D205/08 ,  C07D503/00 ,  C07F7/18 ,  C07D405/12 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07F7/186 ,  C07D205/08 ,  C07D503/00

摘要： .beta.-Lactam compounds of the formula (I) ##STR1## (wherein R represents an esterified carboxyl group, --NR.sup.1 R.sup.2 R.sup.3 represents the residue of a nitrogen base, and R.sup.4 represents a hydrogen atom, a hydroxyl group or acylated or etherified hydroxyl group or the residue of a sulphur nucleophile) are disclosed, together with processes for their preparation. The compounds are valuable intermediates for the preparation or purification of further .beta.-lactam compounds having .beta.-lactamase inhibitory activity.

摘要翻译： 式（I）的β-内酰胺化合物（I）（其中R表示酯化的羧基，-NR 1 R 2 R 3表示氮基的残基，R 4表示氢原子，羟基或酰化或醚化的羟基 基团或硫亲核试剂的残基）及其制备方法。 该化合物是制备或纯化具有β-内酰胺酶抑制活性的其它β-内酰胺化合物的有价值的中间体。

公开(公告)号：US5057496A

公开(公告)日：1991-10-15

申请号：US280495

申请日：1988-12-06

申请人： Peter C. Cherry ,  Michael W. Foxton ,  Barry E. Ayres ,  Andrew D. Searle

发明人： Peter C. Cherry ,  Michael W. Foxton ,  Barry E. Ayres ,  Andrew D. Searle

IPC分类号： C12N9/99 ,  A61K38/55 ,  A61P5/38 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P27/02 ,  A61P27/06 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81

CPC分类号： C07K5/0227 ,  C07K5/0207

摘要： There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 (where R.sup.6 is a hydrogen atom or a hydroxyl group and R.sup.7 is a pyridinyl ring);X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4, and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.Compositions containing the compounds of formula (1) and processes for preparing the compounds are also described.

公开(公告)号：US4230622A

公开(公告)日：1980-10-28

申请号：US749368

申请日：1976-12-10

申请人： Peter C. Cherry ,  Gordon I. Gregory ,  Peter Ward

发明人： Peter C. Cherry ,  Gordon I. Gregory ,  Peter Ward

IPC分类号： C07D503/00

CPC分类号： C07D503/00

摘要： Novel halogen derivatives of clavulanic acid are described which are of value in the preparation of a range of clavulins which either inhibit .beta.-lactamases or show activity against strains of both gram-positive and gram-negative bacteria. Processes for preparing the halogen derivatives are described and methods for converting them into the active clavulins are given.

摘要翻译： 描述了克拉维酸的新型卤素衍生物，其在制备一系列克拉维酮中有价值，其可抑制β-内酰胺酶或显示针对革兰氏阳性菌和革兰氏阴性细菌菌株的活性。 描述了制备卤素衍生物的方法和将其转化成活性克拉维酮的方法。

公开(公告)号：US5578630A

公开(公告)日：1996-11-26

申请号：US338510

申请日：1994-11-25

申请人： Peter C. Cherry ,  Michael W. Foxton ,  Andrew T. Merritt

发明人： Peter C. Cherry ,  Michael W. Foxton ,  Andrew T. Merritt

IPC分类号： C07D405/06 ,  A61K31/41 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： This invention relates to heterocyclic compounds which are inhibitors of the enzyme aromatase, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.Particular compounds of the invention are compounds of formula (I) ##STR1## wherein R.sup.1 represents a cyano or nitro group; R.sup.2 represents hydrogen or one or more halogen atoms;R.sup.3 represents a C.sub.1-6 alkyl group and R.sup.4 represents hydrogen or aC.sub.1-6 alkyl group or R.sup.3 and R.sup.4 together represent a C.sub.3-6 cycloalkyl group; andR.sup.5 represents hydrogen or one or more halogen atoms or C.sub.1-6 alkoxy groups and pharmaceutically acceptable salts and solvates thereof.

摘要翻译： PCT No.PCT / EP93 / 01520 Sec。 371日期：1994年11月25日 102（e）日期1994年11月25日PCT提交1993年6月14日PCT公布。 出版物WO93 / 25548 日期1993年12月23日本发明涉及作为芳香酶酶的抑制剂，其制备方法的杂环化合物，含有它们的药物组合物及其在药物中的用途。 本发明的具体化合物是式（I）化合物其中R 1表示氰基或硝基; R2表示氢或一个或多个卤素原子; R3表示C1-6烷基，R4表示氢或C1-6烷基，R3和R4表示C3-6环烷基; 并且R 5表示氢或一个或多个卤素原子或C 1-6烷氧基及其药学上可接受的盐和溶剂化物。

公开(公告)号：US4290949A

公开(公告)日：1981-09-22

申请号：US809915

申请日：1977-06-24

申请人： Peter C. Cherry ,  Christopher E. Newall ,  Nigel S. Watson ,  Gordon I. Gregory ,  Peter Ward

发明人： Peter C. Cherry ,  Christopher E. Newall ,  Nigel S. Watson ,  Gordon I. Gregory ,  Peter Ward

IPC分类号： C07D503/00 ,  C07D498/04

CPC分类号： C07D503/00

摘要： 2-Vinylclavem compounds are disclosed which have been found of value in the synthesis of thio-derivatives of clavulanic acid which possess antibiotic and .beta.-lactamase inhibitory activity. Methods for preparing the vinylclavem compounds are disclosed and processes for preparing the thio-derivatives are given.

摘要翻译： 公开了已经发现在合成具有抗生素和β-内酰胺酶抑制活性的克拉维酸硫代衍生物中有价值的2-乙烯基化合物。 公开了制备乙烯基化合物的方法，并给出了制备硫代衍生物的方法。